> Trialight public data. Index of pages: https://trialight.com/llms.txt
> Web page: https://trialight.com/data/asset/aticaprant-5a0c94c9-c664-4e37-a5c1-108c48fb2696
> Record changed: 2026-11-04

# Aticaprant

Highest phase reached

Phase 3

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL1921847)

Drug type

Small molecule

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL1921847)

## Development status

**Listing at source**

Listed

**Highest phase reached**

Phase 3

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL1921847)

## Names and chemistry

**Drug type**

Small molecule

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL1921847)

**Drug name**

Aticaprant

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL1921847)

**Molecular weight**

418.51

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL1921847)

**Structure (SMILES)**

Cc1cc(C)cc(\[C@@H\]2CCCN2Cc2ccc(Oc3ccc(C(N)=O)cc3F)cc2)c1

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL1921847)

### Other names (25)

- aticaprant
- Aticaprant
- aticaprant \[INN\]
- ATICAPRANT \[USAN\]
- Aticaprant \[WHO-DD\]
- aticaprant inn
- aticaprant usan
- aticaprant who dd
- cerc 501
- Cerc-501
- CERC-501
- jnj 67953964
- jnj 67953964 aaa
- Jnj-67953964
- JNJ-67953964
- JNJ-67953964-AAA
- jspa 0658
- JSPA-0658
- jspa0658
- JSPA0658
- ly 2456302
- LY-2456302
- ly2456302
- Ly2456302
- LY2456302

## Identifiers

**CAS registry numbers**

- 1174130-61-0

**ChEMBL ID**

CHEMBL1921847

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL1921847)

**InChIKey**

ZHPMYDSXGRRERG-DEOSSOPVSA-N

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL1921847)

**PubChem compound IDs**

- 44129648

**FDA ingredient codes (UNII)**

- DE4G8X55F5

## Regulatory information

### Other regulatory facts

**First in class**

No

**Orphan designation**

No

## Pharmacology

### Drug classification

**Pharmacology name**

aticaprant

**Type**

Synthetic organic

**Drug name stem**

\-caprant

### Mechanisms of action (5)

- **Action**  
Antagonist

**Action type**  
Antagonist

**Target**  
μ receptor

**Gene symbol**  
OPRM1

**Protein identifier**  
P35372

**Median affinity**

7.62

**Affinity units**  
pKi
- **Action**  
Antagonist

**Action type**  
Antagonist

**Target**  
δ receptor

**Gene symbol**  
OPRD1

**Protein identifier**  
P41143

**Median affinity**

6.81

**Affinity units**  
pKi
- **Action**  
Antagonist

**Action type**  
Antagonist

**Target**  
κ receptor

**Gene symbol**  
OPRK1

**Protein identifier**  
P41145

**Median affinity**

9.09

**Affinity units**  
pKB

**Primary target**  
Yes
- **Action**  
Antagonist

**Action type**  
Antagonist

**Target**  
κ receptor

**Gene symbol**  
OPRK1

**Protein identifier**  
P41145

**Median affinity**

9.09

**Affinity units**  
pKi

**Primary target**  
Yes
- **Mechanism**  
Kappa opioid receptor antagonist

**Action type**  
Antagonist

**Target**  
Kappa-type opioid receptor

**Protein identifier**  
P41145

### Open Targets mechanisms

- **Mechanism**  
Kappa opioid receptor antagonist

**Action type**  
Antagonist

**Target**  
Kappa-type opioid receptor

### Investigated indications (5)

- **Condition**  
Depressive Disorder, Major

**Highest recorded phase**  
3

**Condition identifier**  
EFO:0003761

**Subject identifier**  
D003865
- **Condition**  
Tobacco Use Disorder

**Highest recorded phase**  
2

**Condition identifier**  
EFO:0003768

**Subject identifier**  
D014029
- **Condition**  
Anxiety

**Highest recorded phase**  
1

**Condition identifier**  
EFO:0005230

**Subject identifier**  
D001007
- **Condition**  
Depressive Disorder, Treatment-Resistant

**Highest recorded phase**  
2

**Condition identifier**  
EFO:0009854

**Subject identifier**  
D061218
- **Condition**  
Depressive Disorder, Major

**Highest recorded phase**  
3

**Condition identifier**  
MONDO:0002009

**Subject identifier**  
D003865

### Open Targets indications (19)

- **Condition identifier**  
EFO\_0003768

**Highest recorded phase**  
2
- **Condition identifier**  
EFO\_0004318

**Highest recorded phase**  
2
- **Condition identifier**  
EFO\_0009854

**Highest recorded phase**  
2
- **Condition identifier**  
HP\_0000739

**Highest recorded phase**  
1
- **Condition identifier**  
HP\_0000739

**Highest recorded phase**  
2
- **Condition identifier**  
MONDO\_0001247

**Highest recorded phase**  
2
- **Condition identifier**  
MONDO\_0001442

**Highest recorded phase**  
2
- **Condition identifier**  
MONDO\_0001942

**Highest recorded phase**  
2
- **Condition identifier**  
MONDO\_0002009

**Highest recorded phase**  
3
- **Condition identifier**  
MONDO\_0002050

**Highest recorded phase**  
2
- **Condition identifier**  
MONDO\_0004985

**Highest recorded phase**  
2
- **Condition identifier**  
MONDO\_0005146

**Highest recorded phase**  
2
- **Condition identifier**  
MONDO\_0005371

**Highest recorded phase**  
1
- **Condition identifier**  
MONDO\_0005383

**Highest recorded phase**  
2
- **Condition identifier**  
MONDO\_0007079

**Highest recorded phase**  
2
- **Condition identifier**  
MONDO\_0008114

**Highest recorded phase**  
2
- **Condition identifier**  
MONDO\_0008575

**Highest recorded phase**  
2
- **Condition identifier**  
MONDO\_0011918

**Highest recorded phase**  
1
- **Condition identifier**  
MONDO\_0012000

**Highest recorded phase**  
2

### Trial references (6)

- NCT01913535  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT01913535)
- NCT02218775  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT02218775)
- NCT02641028  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT02641028)
- NCT02800928  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT02800928)
- NCT03559192  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT03559192)
- NCT05518149  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT05518149)

## Chemical properties

**Hydrogen bond acceptors**

3

**Hydrogen bond donors**

1

**Polar surface area**

55.56

**Calculated partition coefficient (ALogP)**

5.67

**Calculated partition coefficient (XLogP)**

5

**Prodrug**

No

**Chirality**

Single enantiomer

**Inorganic**

No

**Rule-of-five violations**

1

**Rotatable bonds**

6

**Heavy atoms**

31

**Molecular formula**

C26H27FN2O2

**Monoisotopic mass**

418.20565627

**Natural product**

No

## Evidence counts

**Recorded assays**

65

**Active assays**

23

### Active assay types (2)

- Confirmatory
- Other

## Pharmacologic actions

- Narcotic Antagonists  
Source: [id.nlm.nih.gov](https://id.nlm.nih.gov/mesh/D009292.html)

## Biological measurements

### Observed measurements

#### Oral bioavailability

**Median**

25.2

**Mean**

25.2

**Minimum**

25

**Maximum**

25.4

**Unit**

%

**Assays**

4

**Standard deviation**

0.23094

**Summary method**

median

**Censored results excluded**

0

**Other units excluded**

0

**Unknown units excluded**

0

#### Measurement types

- F

## Related records

### Trials (16)

- A Study in a Human Laboratory Model of Smoking Behavior
- A Study of 14C JNJ-67953964 in Healthy Adult Male Participants
- A Study of Aticaprant 10 mg as Adjunctive Therapy in Adult Participants With Major Depressive Disorder (MDD) With Moderate-to-severe Anhedonia and Inadequate Response to Current Antidepressant Therapy and Long-term Extension Treatment With Aticaprant
- A Study of Aticaprant 10 Milligrams (mg) as Adjunctive Therapy in Adult Participants With MDD With Moderate-to-severe Anhedonia and Inadequate Response to Current Antidepressant Therapy
- A Study of Aticaprant as Adjunctive Therapy in Adult Participants With Major Depressive Disorder (MDD) With Moderate-to-severe Anhedonia and Inadequate Response to Current Antidepressant Therapy
- [A Study of Aticaprant in Adult and Elderly Participants With Major Depressive Disorder (MDD)](https://trialight.com/data/trial/a-study-of-aticaprant-in-adult-and-elderly-participants-with-59ff774f-1f7b-43dc-b9f9-805262dfafc2.md)
- A Study of Aticaprant Plus an Antidepressant to Prevent Return of Depression Symptoms in Participants With Major Depressive Disorder Who Experience a Loss of Interest and Pleasure
- A Study of JNJ-67953964 in Healthy Japanese Adult Male Participants
- A Study of the Feasibility, Safety and Tolerability of Aticaprant as Adjunctive Treatment in Participants With Schizophrenia
- A Study to Explore the Efficacy of JNJ-67953964 in the Treatment of Depression
- A Study to Investigate the Effect of JNJ-67953964 on Gastric Mucosal Integrity in Healthy Male and Female Participants
- A Thorough QT Study of Aticaprant (JNJ-67953964) in Healthy Adult Participants
- Does CERC-501 Attenuate Stress-precipitated Smoking Lapse?
- Fast-Fail Trials in Mood and Anxiety Spectrum Disorders; Kappa Opioid Receptor Phase 2a
- FASTMAS (Fast-Fail Trials in Mood and Anxiety Spectrum Disorders) Kappa Opioid Receptor Phase 1 Study
- Proof-of-Concept Trial of CERC-501 Augmentation of Antidepressant Therapy in Treatment-Resistant Depression

### In development for (14)

- Alcohol dependence Phase 2
- Anxiety Phase 1
- [Bipolar disorder](https://trialight.com/data/condition/bipolar-disorder-a61ecd6f-6fb9-5323-bc0d-ebf861411d3c.md) Phase 2
- [Depressive disorder](https://trialight.com/data/condition/depressive-disorder-7618feda-3f90-5521-94e1-99f7100e8324.md) Phase 2
- Dysthymic disorder Phase 2
- [Generalized anxiety disorder](https://trialight.com/data/condition/generalized-anxiety-disorder-06f2f230-65ba-5929-af6a-36d14f38281d.md) Phase 2
- [Major depressive disorder](https://trialight.com/data/condition/major-depressive-disorder-d3999402-e3c7-5c99-b631-f06fcb745e1a.md) Phase 3
- [Mood disorder](https://trialight.com/data/condition/mood-disorder-00c37338-ecb8-5997-bb93-d0ec3e6e3573.md) Phase 1
- Nicotine dependence Phase 2
- Obsessive-compulsive disorder Phase 2
- Panic disorder Phase 2
- Post-traumatic stress disorder Phase 2
- Social phobia Phase 2
- Specific phobia Phase 2

### Targets (3)

- [OPRD1](https://trialight.com/data/target/oprd1-5ce8b0d6-c823-51ce-a7b3-812976633078.md)
- [OPRK1](https://trialight.com/data/target/oprk1-7b0a0fa0-a4b4-537b-bd00-d871256424e5.md) Kappa opioid receptor antagonist
- [OPRM1](https://trialight.com/data/target/oprm1-04284660-78ba-5225-a86d-21f8a7325d8f.md)

---

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